IP Library Granted Patent US 12,180,525
Granted Patent B2
US 12,180,525 · App. 17/846,935 · Granted Dec 31, 2024

Methods of producing nor-opioid and nal-opioid benzylisoquinoline alkaloids

Inventors: Christina D. Smolke (Menlo Park, CA); Catherine Thodey (Mountain View, CA); Isis Trenchard (Redwood City, CA)
Assignee: Antheia, Inc.
C12P17/182C12N9/0006C12N9/0028C12N9/0071C12N9/14C12N9/90C12N15/85C12P17/12C12P17/18C12Y105/01027C12Y114/16002C12Y114/21004C12N2015/8518C12Y305/04016
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Quick Facts
Patent No.
US 12,180,525
App. No.
17/846,935
Granted
Dec 31, 2024
Kind
B2
Abstract

A method of demethylizing an opioid to a nor-opioid is provided. The method comprises contacting an opioid with at least one enzyme. Contacting the opioid with the at least one enzyme converts the opioid to a nor-opioid. A method of converting a nor-opioid to a nal-opioid is provided. The method comprises contacting a nor-opioid with at least one enzyme. Contacting the nor-opioid with the at least one enzyme converts the nor-opioid to a nal-opioid.

Claims (6)

1. A composition comprising a nal-opioid compound that does not contain one or more detectable impurities associated with chemical synthesis, wherein the one or more detectable impurities associated with chemical synthesis comprises 15,16-Dehydrobuprenorphine, 17,18-Dehydrobuprenorphine, 18,19-demethylbuprenorphine, 19,19′-Ethylbuprenorphine, 2,2′-Bisbuprenorphine, 3-Dehydroxybuprenorphine, 3-O-Methylbuprenorphine, 3-O-Methyl-N-cyanonorbuprenorphine, 3-O-Methyl-N-methylnorbuprenorphine, 6-O-Desmethylbuprenorphine, Buprenorphine N-oxide, N-But-3-enylnorbuprenorphine, N-But-3-enylnormethylbuprenorphine, N-Butylnorbuprenorphine, N-Methylbuprenorphine, Norbuprenorphine, Tetramethylfuran buprenorphine, 1-Bromooxymorphone, 6-Beta oxymorphol, 10-Alpha-hydroxyoxymorphone, 10-Ketooxymorphone, 2,2-Bisoxymorphone, Noroxymorphone, Oxymorphone N-oxide, 10-Hydroxyoxymorphone, 4-Hydroxyoxymorphone, 8-Hydroxyoxymorphone, Hydromorphinol, 10-Hydroxynaltrexone, 10-Ketonaltrexone, 14-Hydroxy-17-cyclopropylmethylnormorphinone, 2,2′-Bisnaltrexone, 3-Cyclopropylmethylnaltrexone, 3-O-Methylnaltrexone, 8-Hydroxynaltrexone, N-(3-Butenyl)-noroxymorphone, Naltrexone aldol dimer, N-Formyl-noroxymorphone, 10-Alpha-hydroxynaloxone, 10-Beta-hydroxynaloxone, 10-Ketonaloxone, 3-O-Allylnaloxone, 7,8-Didehydronaloxone, 2,2′-Bisnaloxone, Naloxone N-oxide, Beta-epimer of nalbuphine, 2,2′-Bisnalbuphine, 6-Ketonalbuphine, 10-Ketonalbuphine, Alpha-noroxymorphol, N-(Cyclobutylcarbonyl)-alpha-noroxymorphol, or N-Formyl-6-alpha-noroxymophol.

2. The composition of claim 1 , wherein the nal-opioid is buprenorphine and the one or more impurities associated with chemical synthesis comprise 15,16-Dehydrobuprenorphine, 17,18-Dehydrobuprenorphine, 18,19-demethylbuprenorphine, 19,19′-Ethylbuprenorphine, 2,2′-Bisbuprenorphine, 3-Deshydroxybuprenorphine, 3-O-Methylbuprenorphine, 3-O-Methyl-N-cyanonorbuprenorphine, 3-O-Methyl-N-methylnorbuprenorphine, 6-O-Desmethylbuprenorphine, Buprenorphine N-oxide, N-But-3-enylnorbuprenorphine, N-But-3-enylnormethylbuprenorphine, N-Butylnorbuprenorphine, N-Methylbuprenorphine, Norbuprenorphine, and Tetramethylfuran buprenorphine.

3. The composition of claim 1 , wherein the nal-opioid is oxymorphone and the one or more impurities associated with chemical synthesis comprise 1-Bromooxymorphone, 6-Beta oxymorphol, 10-Alpha-hydroxyoxymorphone, 10-Ketooxymorphone, 2,2-Bisoxymorphone, Noroxymorphone, Oxymorphone N-oxide, 10-Hydroxyoxymorphone, 4-Hydroxyoxymorphone, 8-Hydroxyoxymorphone, and Hydromorphinol.

4. The composition of claim 1 , wherein the nal-opioid is naltrexone and the one or more impurities associated with chemical synthesis comprise 10-Hydroxynaltrexone, 10-Ketonaltrexone, 14-Hydroxy-17-cyclopropylmethylnormorphinone, 2,2′-Bisnaltrexone, 3-Cyclopropylmethylnaltrexone, 3-O-Methylnaltrexone, 8-Hydroxynaltrexone, N-(3-Butenyl)-noroxymorphone, Naltrexone aldol dimer, or N-Formyl-noroxymorphone.

5. The composition of claim 1 , wherein the nal-opioid is naloxone and the one or more impurities associated with chemical synthesis comprise 10-Alpha-hydroxynaloxone, 10-Beta-hydroxynaloxone, 10-Ketonaloxone, 3-O-Allylnaloxone, 7,8-Didehydronaloxone, 2,2′-Bisnaloxone, and Naloxone N-oxide.

6. The composition of claim 1 , wherein the nal-opioid is nalbuphine and the one or more impurities associated with chemical synthesis comprise Beta-epimer of nalbuphine, 2,2′-Bisnalbuphine, 6-Ketonalbuphine, 10-Ketonalbuphine, Alpha-noroxymorphol, N-(Cyclobutylcarbonyl)-alpha-noroxymorphol, and N-Formyl-6-alpha-noroxymophol.

Assignments (2)
SECURITY INTEREST Recorded Aug 29, 2025
From: ANTHEIA, INC.
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 072750/0812 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 15, 2023
From: SMOLKE, CHRISTINA D.; THODEY, CATHERINE; TRENCHARD, ISIS
To: ANTHEIA, INC.
Reel/Frame 063102/0618 →
Continuity (6)
Continuation 16918529 · Jul 1, 2020
Continuation 16127084 · Sep 10, 2018
Continuation PCTUS2017057237 · Oct 18, 2017
Provisional Application 62409837 · Oct 18, 2016
Provisional Application 62473215 · Mar 17, 2017
Related Publication 20230104286A1 · Apr 6, 2023